K., Misaki, KentaroMisaki, KentaroK.N.M., Tue, Nguyen MinhTue, Nguyen MinhN.M.T., Takamura-Enya, TakejiTakamura-Enya, TakejiT.H., Takigami, HidetakaTakigami, HidetakaH.G., Suzuki, GoSuzuki, GoG.L.H., Tuyen, Le HuuTuyen, Le HuuL.H.S., Takahashi, ShinTakahashi, ShinS.S., Tanabe, ShinsukeTanabe, ShinsukeS.2025-09-052025-09-05202310.3390/ijerph20010080https://scholar.vnu.edu.vn/handle/123456789/8294To establish the risk of the endocrine disrupting activity of polycyclic aromatic compounds, especially oxygenated and nitrated polycyclic aromatic hydrocarbons (oxy-PAHs and nitro-PAHs, respectively), antiandrogenic and estrogenic activities were determined using chemically activated luciferase expression (CALUX) assays with human osteoblast sarcoma cells. A total of 27 compounds including 9 oxy-PAHs (polycyclic aromatic ketones and quinones) and 8 nitro-PAHs was studied. The oxy-PAHs of 7H-benz[de]anthracen-7-one (BAO), 11H-benzo[a]fluoren-11-one (B[a]FO), 11H-benzo[b]fluoren-11-one (B[b]FO), and phenanthrenequinone (PhQ) exhibited significantly the potent inhibition of AR activation. All nitro-PAHs exhibited high antiandrogenic activities (especially high for 3-nitrofluoranthene (3-NFA) and 3-nitro-7H-benz[de]anthracen-7-one (3-NBAO)), and the AR inhibition was confirmed as noncompetitive for 3-NFA, 3-NBAO, and 1,3-dinitropyrene (1,3-DNPy). Antiandrogenic activity of 3-NFA demonstrated characteristically a U-shaped dose–response curvehowever, the absence of fluorescence effect on the activity was confirmed. The prominent estrogenic activity dependent on dose–response curve was confirmed for 2 oxy-PAHs (i.e., B[a]FO and B[b]FO). Elucidating the role of AR and ER on the effects of polycyclic aromatic compounds (e.g., oxy- and nitro-PAHs) to endocrine dysfunctions in mammals and aquatic organisms remains a challenge. © 2023 Elsevier B.V., All rights reserved.EnglishAntiandrogenic ActivityChemically Activated Luciferase Expression AssayEstrogenic ActivityNitrated Polycyclic Aromatic HydrocarbonPolycyclic Aromatic KetonePolycyclic Aromatic Quinone1 NitropyreneAndrostanoloneBenz[a]anthraceneChryseneEstradiolGlyceryl TrinitratePhenanthrenePhenanthrenequinoneTestosteroneLuciferasesNitratesPolycyclic Aromatic HydrocarbonsPolycyclic CompoundsQuinones1 Nitropyrene3 NitrofluorantheneAndrogen ReceptorAndrostanoloneBenz[a]anthraceneChryseneEstradiolGlyceryl TrinitrateKetoneLuciferasePhenanthrenePhenanthrenequinonePolycyclic Aromatic HydrocarbonQuinone DerivativeTestosteroneUnclassified DrugNitric Acid DerivativePolycyclic HydrocarbonAndrogenDose-response RelationshipEndocrine DisruptorEstrogenic CompoundGene ExpressionInhibitionNitratePahReaction KineticsRisk AssessmentAnimal CellArticleBinding AffinityChemical StructureCognitionCytotoxicityEnvironmental FactorEstrogen ActivityGenetic TranscriptionHumanHydrogen BondMouseMutagenicityNonhumanObesityOocyte MaturationOxidative StressReproductive HealthSexual FunctionSpermatogenesisSpermatozoon DensityAnimalChemistryMammalAnimalsHumansLuciferasesMammalsNitratesPolycyclic Aromatic HydrocarbonsPolycyclic CompoundsQuinonesArticle